Polyols, such as cyclodextrins, sugars, and other carbohydrates are used in tablets containing pharmaceutically active agents for various purposes, such as for taste-masking purposes in chewable tablets or for bulk filling purposes in fast dissolving tablets. The pharmaceutically active agent cetirizine, however, is both bitter and highly susceptible to degradation by esterification with polyols. PCT Patent Application WO 03/059328 discloses that esterification of cetirizine can be controlled by creating a very dry environment and/or by physical separation of cetirizine and polyols in the tablet. However, such a process fail to create an effective environment for taste-masking purposes, as the resulting tablet will have an initial taste of bitterness as the cetirizine must initially dissolve in the mouth prior to initiation of the “in-situ” taste-masking effect of the polyol in the tablet.
Applicants, however, have unexpectedly found a process by which that cetirizine and polyols can be physically combined for use in a tablet without causing a significant esterification to the cetirizine. Specifically, it has been unexpectedly found that the addition of an alkalizing agent coupled with a wet formulation process allows for the presence of cetirizine and polyols together in the same formulation, and further unexpectedly at levels higher than ten molar equivalents as is specified in PCT Patent Application WO 03/059328. By combining cetirizine and polyols in a wet formulation, it is now possible for cetirizine-polyol complexation to occur during the manufacturing process of the tablet, thereby eliminating the drawbacks of the above-discussed in-situ complexation.